和螺旋环N-异环的单步合成,使用斯坦尼尔胺协议 (SnAP) 试剂和子
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Updated: Apr 19, 2026
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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
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Woon-Yew Siau1, Jeffrey W Bode
1Laboratorium für Organische Chemie, Department of Chemistry and Applied Biosciences, ETH-Zürich , 8093 Zürich, Switzerland.
Journal of the American Chemical Society
|December 9, 2014
概括
一种新方法将循环和斯坦尼尔胺协议 (SnAP) 试剂结合起来,以创建有价值的螺旋循环胺支架. 这种高效的合成为药物发现和开发开辟了新的途径.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 合成化学 合成化学
背景情况:
- 螺旋环N-异环环是药物发现中的关键支架.
- 现有的合成方法可能缺乏效率或简单性.
- 对于进一步的功能化,N-无保护氨基是特别可取的.
研究的目的:
- 开发一种操作上简单的方法来合成和的螺旋环N-异环环.
- 探索斯坦尼尔胺协议 (SnAP) 试剂在异环合成中的实用性.
- 为了产生新的α-trifluoromethylmorpholine和piperazine衍生物.
主要方法:
- 循环子与SNAP试剂的反应.
- 使用非循环三甲基基与SNAP试剂.
- 合成的螺旋环胺的特征.
主要成果:
- 成功合成和的螺旋环N-异环环.
- 产生N-无保护的螺旋环胺.
- 从非循环三甲基基中形成α-三甲基形态素和piperazines.
结论:
- SnAP协议提供了一条有效的途径,以获得有价值的螺旋环胺基架.
- 这种方法促进了药物发现关键中间体的合成.
- 该协议是多功能性的,产生一般的螺旋环胺和特定的α-CF3异循环.
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